Cholesteryl ester transfer protein and its inhibitors
Sudichhya Shrestha1, Ben J Wu1, Liam Guiney2
1School of Medical Sciences, University of New South Wales Sydney, Sydney, New South Wales, Australia.
Journal of Lipid Research
|March 1, 2018
Summary
Inhibiting cholesteryl ester transfer protein (CETP) increases HDL-cholesterol and lowers LDL-cholesterol, potentially reducing cardiovascular disease. Small molecule inhibitors have been evaluated in major clinical trials.
Area of Science:
- Biochemistry
- Cardiovascular Medicine
- Pharmacology
Background:
- Cholesterol metabolism is crucial for cardiovascular health.
- Cholesteryl ester transfer protein (CETP) facilitates lipid transfer between lipoproteins.
- CETP activity influences HDL-cholesterol and LDL-cholesterol levels.
Purpose of the Study:
- To review the structure and mechanism of CETP.
- To discuss CETP regulation and non-lipid transport functions.
- To summarize clinical trial outcomes of CETP inhibitors.
Main Methods:
- Review of existing literature on CETP structure, function, and regulation.
- Analysis of data from large-scale cardiovascular clinical outcome trials of small molecule CETP inhibitors.
Main Results:
- CETP mediates bidirectional transfer of cholesteryl esters and triglycerides.
- Inhibition of CETP increases HDL-cholesterol and decreases LDL-cholesterol.
- Four small molecule CETP inhibitors have undergone extensive clinical outcome trials.
Conclusions:
- CETP inhibition shows potential for reducing atherosclerotic cardiovascular disease.
- Understanding CETP's role is key to developing novel lipid-lowering therapies.
- Clinical trial results provide insights into the therapeutic efficacy of CETP inhibitors.
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